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Titolo:
EXHIBITION OF ANTIPLATETLET EFFECT OF ISOCARBACYCLIN METHYL-ESTER ANDITS FREE ACID VIA AN INCREASE IN CAMP IN PLATELETS
Autore:
AOKI Y; INOUE K; KITAHARA S; KIYOKI M; ARAKI H;
Indirizzi:
TEIJIN LTD,TEIJIN INST BIOMED RES,PHARMACEUT DEV RES LABS,PHARMACOL RES DEPT,4-3-2 ASAHIGAOKA HINO TOKYO 191 JAPAN TAISHO PHARMACEUT CO LTD,RES CTR,DEPT PHARMACOL 2 OMIYA SAITAMA JAPAN
Titolo Testata:
Arzneimittel-Forschung
fascicolo: 9, volume: 45-2, anno: 1995,
pagine: 970 - 974
SICI:
0004-4172(1995)45-2:9<970:EOAEOI>2.0.ZU;2-R
Fonte:
ISI
Lingua:
ENG
Soggetto:
PROSTAGLANDIN-I2 ANALOG; EXPERIMENTAL-ANIMALS; PROSTACYCLIN ANALOG; OP-41483; RECEPTOR; CELLS;
Keywords:
CAS 88911-35-7; CAS 88931-51-5; ISOCARBACYCLIN METHYL ESTER, FREE ACID; PLATELETS, CAMP LEVEL; TEI-7165, PHARMACOLOGY; TEI-9090, PHARMACOLOGY;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
18
Recensione:
Indirizzi per estratti:
Citazione:
Y. Aoki et al., "EXHIBITION OF ANTIPLATETLET EFFECT OF ISOCARBACYCLIN METHYL-ESTER ANDITS FREE ACID VIA AN INCREASE IN CAMP IN PLATELETS", Arzneimittel-Forschung, 45-2(9), 1995, pp. 970-974

Abstract

Isocarbacyclin methyl ester (CAS 88931-51-5, TEI-9090) and its free acid (CAS 88911-35-7, TEI-7165) are chemically stable analogues of prostaglandin (PGI I-2. The cAMP increasing activities of TEI-9090 and TEI-7165 were investigated. TEI-9090, TEI-7165, PGI(2), and PGE(1) causedthe accumulation of cAMP in rabbit and human platelets. The effects of TEI-9090, TEI-7165, and PGE(1) were longer lasting than the effect of PGI(2). Each drug concentration-dependently increased the cAMP levelin rabbit and human platelets. The order of cAMP-increasing activity,vas PGI(2) > PGE(1) = TEI-9090 = TEI-7165 in rabbit platelets and PGI(2) > TEI-9090 = TEI-7165 > PGE(1) in human platelets. The antiplateletaggregation activity of TEI-9090 in rabbit and human platelets was remarkably decreased by the addition of an esterase inhibitor, diisopropyl fluorophosphate (DFP). However, this activity of TEI-7165 was not affected by the inhibitor In the presence of DFP, the cAMP accumulationby TEI-9090 in rabbit platelets was almost completely inhibited but that by TEI-7165 was not inhibited. These results suggest that TEI-9090is deesterified to TEI-7165 and that this fr,ee acid then inhibits platelet aggregation via an inn ease in the cAMP level in the platelets.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 02/10/20 alle ore 02:02:59